GSK1482160

    WARNING: This product is for research use only, not for human or veterinary use.

Hodoodo CAT#: H530649

CAS#: 1001389-72-5

Description: GSK1482160 is a potent and selective P2X7 receptor allosteric modulator with nanomolar binding affinity and high selectivity. GSK1482160 has been successfully radiolabeled and utilized for imaging P2X7 levels in a mouse model of lipopolysaccharide-induced systemic inflammation.

Chemical Structure

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GSK1482160
CAS# 1001389-72-5
Instruction

Theoretical Analysis

Hodoodo Cat#: H530649
Name: GSK1482160
CAS#: 1001389-72-5
Chemical Formula: C14H14ClF3N2O2
Exact Mass: 334.07
Molecular Weight: 334.723
Elemental Analysis: C, 50.24; H, 4.22; Cl, 10.59; F, 17.03; N, 8.37; O, 9.56

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Related CAS #: 1695551-19-9 (isomer)   1001389-72-5    

Synonym: GSK1482160; GSK-1482160; GSK 1482160.

IUPAC/Chemical Name: (S)-N-(2-chloro-3-(trifluoromethyl)benzyl)-N-methyl-5-oxopyrrolidine-2-carboxamide

InChi Key: IHRKNQDNYKZPNL-JTQLQIEISA-N

InChi Code: InChI=1S/C14H14ClF3N2O2/c1-20(13(22)10-5-6-11(21)19-10)7-8-3-2-4-9(12(8)15)14(16,17)18/h2-4,10H,5-7H2,1H3,(H,19,21)/t10-/m0/s1

SMILES Code: ClC1=C(C=CC=C1CN(C([C@@H]2CCC(N2)=O)=O)C)C(F)(F)F

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 334.72 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Han J, Liu H, Liu C, Jin H, Perlmutter JS, Egan TM, Tu Z. Pharmacologic characterizations of a P2X7 receptor-specific radioligand, [11C]GSK1482160 for neuroinflammatory response. Nucl Med Commun. 2017 May;38(5):372-382. doi: 10.1097/MNM.0000000000000660. PubMed PMID: 28338530; PubMed Central PMCID: PMC5401628.

2: Territo PR, Meyer JA, Peters JS, Riley AA, McCarthy BP, Gao M, Wang M, Green MA, Zheng QH, Hutchins GD. Characterization of (11)C-GSK1482160 for Targeting the P2X7 Receptor as a Biomarker for Neuroinflammation. J Nucl Med. 2017 Mar;58(3):458-465. doi: 10.2967/jnumed.116.181354. Epub 2016 Oct 20. PubMed PMID: 27765863.

3: Gao M, Wang M, Green MA, Hutchins GD, Zheng QH. Synthesis of [(11)C]GSK1482160 as a new PET agent for targeting P2X(7) receptor. Bioorg Med Chem Lett. 2015 May 1;25(9):1965-70. doi: 10.1016/j.bmcl.2015.03.021. Epub 2015 Mar 14. PubMed PMID: 25819093.

4: Solini A, Usuelli V, Fiorina P. The dark side of extracellular ATP in kidney diseases. J Am Soc Nephrol. 2015 May;26(5):1007-16. doi: 10.1681/ASN.2014070721. Epub 2014 Dec 1. Review. PubMed PMID: 25452669; PubMed Central PMCID: PMC4413770.

5: Ochoa-Cortes F, Liñán-Rico A, Jacobson KA, Christofi FL. Potential for developing purinergic drugs for gastrointestinal diseases. Inflamm Bowel Dis. 2014 Jul;20(7):1259-87. doi: 10.1097/MIB.0000000000000047. Review. PubMed PMID: 24859298; PubMed Central PMCID: PMC4340257.

6: Ali Z, Laurijssens B, Ostenfeld T, McHugh S, Stylianou A, Scott-Stevens P, Hosking L, Dewit O, Richardson JC, Chen C. Pharmacokinetic and pharmacodynamic profiling of a P2X7 receptor allosteric modulator GSK1482160 in healthy human subjects. Br J Clin Pharmacol. 2013 Jan;75(1):197-207. doi: 10.1111/j.1365-2125.2012.04320.x. PubMed PMID: 22568863; PubMed Central PMCID: PMC3555059.